RS 127445 hydrochloride
Chemical Name: 4-(4-Fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine hydrochloride
Purity: ≥98%
Biological Activity
RS 127445 hydrochloride is a high affinity 5-HT2B receptor antagonist (pKi = 9.5). Displays 1000-fold selectivity for 5-HT2B with good bioavailability.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.
Bonhaus et al.
Br.J.Pharmacol., 1999;127:1075 -
Evidence for a control of plasma serotonin levels by 5-Hydroxytryptamine2B receptors in mice.
Callebert et al.
J.Pharmacol.Exp.Ther., 2006;317:724
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Citations for RS 127445 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for RS 127445 hydrochloride include:
8 Citations: Showing 1 - 8
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Pulmonary fibrosis in vivo displays increased p21 expression reduced by 5-HT2B receptor antagonists in vitro - a potential pathway affecting proliferation.
Authors: Lofdahl
Sci Rep 2018;8(1):1927
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Heterodimers of serotonin receptor subtypes 2 are driven by 5-HT2C protomers.
Authors: Moutkine Et al.
J Biol Chem 2017;292:6352
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A human and animal model-based approach to investigating the anti-inflammatory profile and potential of the 5-HT2B receptor antagonist AM1030.
Authors: Palmqvist Et al.
J Inflamm (Lond) 2016;13:20
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Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells.
Authors: Tanaka Et al.
J Biol Chem 2014;289:10466
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Serotonin 2B receptor (5-HT2B R) signals through prostacyclin and PPAR-β/δ in osteoblasts.
Authors: Chabbi-Achengli Et al.
PLoS One 2013;8:e75783
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Identification of new genes involved in human adipogenesis and fat storage.
Authors: Söhle Et al.
PLoS One 2012;7:e31193
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Deconstructing antiobesity compound action: requirement of serotonin 5-HT2B receptors for dexfenfluramine anorectic effects.
Authors: Banas Et al.
Neuropsychopharmacology 2011;36:423
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Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors.
Authors: Murray Et al.
J Neurophysiol 2011;106:925
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